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Multiple-dose phase I study of transnasal butorphanol
W C Shyu1, K A Pittman, D Robinson
1Department of Metabolism and Pharmacokinetics, Bristol-Myers Squibb Pharmaceutical Research Institute, Syracuse, NY 13221.
Clinical Pharmacology and Therapeutics
|July 1, 1993
Summary
Transnasal butorphanol demonstrated good safety and tolerance in a phase I study. Pharmacokinetic analysis revealed dose-proportional absorption and rapid attainment of peak plasma levels.
Area of Science:
- Pharmacology
- Clinical Pharmacology
- Drug Development
Background:
- Transnasal drug delivery offers an alternative route for systemic administration.
- Butorphanol is an opioid agonist-antagonist with analgesic properties.
Purpose of the Study:
- To evaluate the safety, tolerance, and pharmacokinetics of transnasal butorphanol.
- To assess dose-proportionality and steady-state achievement of transnasal butorphanol.
Main Methods:
- Double-blind, multiple-dose phase I study involving 18 subjects.
- Administration of placebo or escalating doses of transnasal butorphanol tartrate.
- Serial blood sampling for pharmacokinetic analysis using radioimmunoassay.
- Nasal examinations to assess local tolerance.
Main Results:
- Butorphanol was rapidly absorbed, with peak plasma levels within 1 hour.
- Pharmacokinetics showed dose-proportional increases in Cmax, Cmin, and AUC.
- Mean elimination half-life was 5.45 hours; steady state was reached within eight doses.
- Transnasal butorphanol was well tolerated with no significant nasal adverse effects.
Conclusions:
- Transnasal butorphanol exhibits favorable safety and tolerance profiles.
- The drug demonstrates predictable pharmacokinetics with dose-proportional absorption.
- Transnasal butorphanol is a viable alternative for butorphanol administration.